SYNTHESIS AND STRUCTURE-ACTIVITY-RELATIONSHIPS OF POTENT RETINOID-X-RECEPTOR LIGANDS

A series of potent retinoid X receptor (RXR) selective ligands was des igned and prepared. The lead compound 7a showed good binding (K-i; 20- 50 nM) and transactivation (EC50; 40-50 nM) to the RXR subfamily of re tinoid receptors. More importantly, small variations in the geometry o f the cyclopentane ring moiety led to 9, one of the most potent RXR ag onists to date (K-i: 3-8 nM; EC50: 3-4 nM). (C) 1997 Elsevier Science Ltd.